AU2017290238B2 - Diprovocims: a new and potent class of TLR agonists - Google Patents

Diprovocims: a new and potent class of TLR agonists Download PDF

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Publication number
AU2017290238B2
AU2017290238B2 AU2017290238A AU2017290238A AU2017290238B2 AU 2017290238 B2 AU2017290238 B2 AU 2017290238B2 AU 2017290238 A AU2017290238 A AU 2017290238A AU 2017290238 A AU2017290238 A AU 2017290238A AU 2017290238 B2 AU2017290238 B2 AU 2017290238B2
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Australia
Prior art keywords
mmol
pyrrolidine
trans
conhch
bis
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AU2017290238A
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AU2017290238A1 (en
Inventor
Bruce Beutler
Dale L. Boger
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Scripps Research Institute
University of Texas System
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Scripps Research Institute
University of Texas System
University of Texas at Austin
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/16Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/10Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/4025Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/04Immunostimulants
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Immunology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pyrrole Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Peptides Or Proteins (AREA)
AU2017290238A 2016-06-29 2017-06-29 Diprovocims: a new and potent class of TLR agonists Active AU2017290238B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662356314P 2016-06-29 2016-06-29
US62/356,314 2016-06-29
PCT/US2017/040028 WO2018005812A1 (en) 2016-06-29 2017-06-29 Diprovocims: a new and potent class of tlr agonists

Publications (2)

Publication Number Publication Date
AU2017290238A1 AU2017290238A1 (en) 2018-12-13
AU2017290238B2 true AU2017290238B2 (en) 2021-02-18

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Family Applications (1)

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AU2017290238A Active AU2017290238B2 (en) 2016-06-29 2017-06-29 Diprovocims: a new and potent class of TLR agonists

Country Status (10)

Country Link
US (1) US11040959B2 (https=)
EP (1) EP3445758B1 (https=)
JP (1) JP6964298B2 (https=)
KR (1) KR102522730B1 (https=)
CN (1) CN109641878B (https=)
AU (1) AU2017290238B2 (https=)
BR (1) BR112018077397A2 (https=)
CA (1) CA3026178C (https=)
IL (1) IL263388B (https=)
WO (1) WO2018005812A1 (https=)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN113164445A (zh) * 2018-08-02 2021-07-23 得克萨斯系统大学评议会 Tlr1/2激动剂地普罗考姆的佐剂作用协同增效检查点抑制性抗体以消除疾病
JP2023527792A (ja) 2020-05-27 2023-06-30 アキシャル セラピューティクス,インク. Tlr2調節剤化合物、医薬組成物、及びそれらの使用
US20250367166A1 (en) * 2022-04-29 2025-12-04 The Scripps Research Institute Next generation diprovocims that activate the innate and adaptive immune response
US20260091126A1 (en) * 2022-09-20 2026-04-02 The Curators Of The University Of Missouri Amino acid-modified lipids for rna delivery

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20100173969A1 (en) * 2001-08-08 2010-07-08 Pepys Mark B Therapeutic agent

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005016235A2 (en) * 2003-04-14 2005-02-24 The Regents Of The University Of California Combined use of impdh inhibitors with toll-like receptor agonists
PE20071079A1 (es) 2005-11-15 2007-12-16 Cytokinetics Inc Compuestos de piperidina como inhibidores de la proliferacion celular
AU2011232421B2 (en) 2010-03-23 2015-08-13 Novartis Ag Compounds (cystein based lipopeptides) and compositions as TLR2 agonists used for treating infections, inflammations, respiratory diseases etc.
EP2958889B1 (en) 2013-02-25 2017-03-22 The Scripps Research Institute Neoseptins: small molecule adjuvants
US9918959B2 (en) 2014-08-06 2018-03-20 The Board Of Regents Of The University Of Texas System TLR-independent small molecule adjuvants

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20100173969A1 (en) * 2001-08-08 2010-07-08 Pepys Mark B Therapeutic agent

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
SCI. ADV., 2015, vol. 1, no. 3, pages 1 - 12 *

Also Published As

Publication number Publication date
CN109641878B (zh) 2021-09-14
CA3026178C (en) 2024-05-21
WO2018005812A1 (en) 2018-01-04
KR20190014133A (ko) 2019-02-11
CA3026178A1 (en) 2018-01-04
IL263388A (en) 2018-12-31
JP6964298B2 (ja) 2021-11-10
EP3445758A1 (en) 2019-02-27
US11040959B2 (en) 2021-06-22
EP3445758A4 (en) 2019-09-25
BR112018077397A2 (pt) 2019-10-01
KR102522730B1 (ko) 2023-04-19
AU2017290238A1 (en) 2018-12-13
CN109641878A (zh) 2019-04-16
JP2019519574A (ja) 2019-07-11
IL263388B (en) 2021-02-28
EP3445758B1 (en) 2020-11-04
US20200207742A1 (en) 2020-07-02

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